Activity-Based Probes for Proteases Pave the Way to Theranostic Applications Article Swipe
Georgia Sotiropoulou
,
Eleni Zingkou
,
Evangelos Bisyris
,
Georgios Pampalakis
·
YOU?
·
· 2022
· Open Access
·
· DOI: https://doi.org/10.3390/pharmaceutics14050977
YOU?
·
· 2022
· Open Access
·
· DOI: https://doi.org/10.3390/pharmaceutics14050977
Proteases are important enzymes in health and disease. Their activities are regulated at multiple levels. In fact, proteases are synthesized as inactive proenzymes (zymogens) that are activated by proteolytic removal of their pro-peptide sequence and can remain active or their activity can be attenuated by complex formation with specific endogenous inhibitors or by limited proteolysis or degradation. Consequently, quite often, only a fraction of the protease molecules is in the active/functional form, thus, the abundance of a protease is not always linearly proportional to the (patho)physiological function(s). Therefore, assays to determine the active forms of proteases are needed, not only in research but also in molecular diagnosis and therapy. Activity-based probes (ABPs) are chemical entities that bind covalently to the active enzyme/protease. ABPs carry a detection tag to enable localization and quantification of specific enzymatic/proteolytic activities with applications in molecular imaging and diagnosis. Moreover, ABPs act as suicide inhibitors of proteases, which can be exploited for delineation of the functional role(s) of a given protease in (patho) biological context and as potential therapeutics. In this sense, ABPs represent new theranostic agents. We outline recent developments pertaining to ABPs for proteases with potential therapeutic applications, with the aim to highlight their importance in theranostics.
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Metadata
- Type
- review
- Language
- en
- Landing Page
- https://doi.org/10.3390/pharmaceutics14050977
- https://www.mdpi.com/1999-4923/14/5/977/pdf?version=1651748967
- OA Status
- gold
- Cited By
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- Related Works
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- OpenAlex ID
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All OpenAlex metadata
Raw OpenAlex JSON
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https://doi.org/10.3390/pharmaceutics14050977Digital Object Identifier
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Activity-Based Probes for Proteases Pave the Way to Theranostic ApplicationsWork title
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reviewOpenAlex work type
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enPrimary language
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2022Year of publication
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2022-04-30Full publication date if available
- Authors
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Georgia Sotiropoulou, Eleni Zingkou, Evangelos Bisyris, Georgios PampalakisList of authors in order
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https://doi.org/10.3390/pharmaceutics14050977Publisher landing page
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https://www.mdpi.com/1999-4923/14/5/977/pdf?version=1651748967Direct link to full text PDF
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goldOpen access status per OpenAlex
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https://www.mdpi.com/1999-4923/14/5/977/pdf?version=1651748967Direct OA link when available
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Proteases, Proteolysis, Protease, Context (archaeology), Biochemistry, Enzyme, Computational biology, Biology, Chemistry, PaleontologyTop concepts (fields/topics) attached by OpenAlex
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12Total citation count in OpenAlex
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2024: 6, 2023: 4, 2022: 2Per-year citation counts (last 5 years)
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10Other works algorithmically related by OpenAlex
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